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Pharmacotherapeutic group: anthelmintic and antiprotozoal agent.
ATX Code: Р02СА03
Albendazole is an anthelmintic drug, the pharmacological properties of which are due to the action of the active substance - albendazole. Albendazole belongs to the group of carbamate benzimidazoles. The mechanism of action of albendazole is its ability to disrupt the activity of the microtubular system of the cells of the intestinal canal of worms, causing damage to the tubulin protein. This results in biochemical disturbances in the cell - inhibition of glucose and fumarate reductose transport, which underlies the suppression of cell division at the metaphase stage and which is associated with the suppression of egg-laying and the development of helminth larvae. Albendazole blocks the movement of secretory granules and other organelles in the muscle cells of roundworms, causing their death.
Albendazole is effective against most intestinal nematodes, as well as larval (larval stages) cestodes, as well as Giardia. Albendazole as an antiparasitic drug has a fairly wide spectrum of action.
Suction. After ingestion, the drug is poorly absorbed in the gastrointestinal tract, in an unchanged form is not detected in the blood plasma. Oral bioavailability is low. Intake of fatty foods increases absorption and maximum concentration 5 times.
Metabolism. Albendazole is rapidly converted in the liver to the primary metabolite - albendazole sulfoxide, which also has anthelmintic activity.
Distribution. The maximum plasma concentration of albendazole sulfoxide is reached 2-5 hours after administration. 70% of the metabolite is associated with plasma proteins and is fully distributed throughout the body: found in urine, bile, liver, in the wall and fluid of cysts of worms, cerebrospinal fluid.
Derivation. Albendazole sulfoxide in the liver is converted to albendazole sulfone (secondary metabolite) and other oxidized products. The half-life of albendazole sulfoxide is 8-12 hours. Excreted through the kidneys in the form of various metabolites. Excretion through the kidneys of albendazole and albendazole sulfoxide is negligible. In patients with impaired renal function, clearance does not change.
In patients with liver damage, bioavailability increases, the maximum concentration of albendazole sulfoxide in the blood plasma increases by 2 times, and the half-life is prolonged.
Albendazole induces cytochrome SUR1A2 in human liver cells, accelerates the metabolism of many drugs.
ascariasis, pathogen - round worms Ascaris lumbricoidesl;
trichocephalosis (whipworm), pathogen - round helminth Trichocephalus trichiurus;
enterobiosis (pinworms), pathogen - round helminth Enterobius vermicularis;
hookworm (hookhead), pathogens - Ancylostoma duodenale and Necator americanus;
trichinosis, pathogen —Trichinella spiralis;
toxocarosis, pathogen - Toxocara canis;
Giardiasis, pathogen - Giardia intestinalis;
Strobiloidosis (intestinal eel), pathogen - round helminth Strongiloides strcoralis, as well as mixed invasions.
- tissue cestodose:
Neurocysticercosis, pathogen Cysticercus cellulosus (larval stage of pork tapeworm);
hydatid echinococcosis of the liver, lungs, peritoneum, pathogen - Echinococcus granulosus (larval stage of canine tapeworm);
as an aid in the surgical treatment of alveolar echinococcosis, the pathogen is Echinococcus multilocularis.
Each tablet film coated contains:
Active ingredient: albendazole -200.00 / 400.00 mg
Excipients: corn starch - 129.70 / 83.00 mg, dried corn starch - 0 / 10.00 mg, sodium lauryl sulfate - 4.00 / 5.00 mg, povidone (polyvinylpyrrolidone K 30) -3.350 / 5.00 mg, methyl parahydroxybenzoate - 0.270 / 0.360 mg, propyl parahydroxybenzoate - 0.030 / 0.040 mg, gelatin - 3.70 / 5.50 mg, purified talc - 6.70 / 10.00 mg, sodium carboxymethyl starch - 3.350 / 5.20 mg, colloidal silicon dioxide - 2.00 / 3,00 mg, magnesium stearate - 2,00 / 3,00 mg.
Shell: hypromellose - 2.40 / 5.32 mg, titanium dioxide - 1.80 / 3.20 mg, purified talc - 1.20 / 1.60 mg, sodium lauryl sulfate - 0.10 / 0 mg, macrogol 400 - 0.500 / 0 mg, propylene glycol - 0 / 1.60 mg.
Albendazole is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
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Dosage and Administration
Inside, during or after meals. Special training and diets are required. Dosage form is chosen individually, depending on the ease of administration of the drug and tolerance of its constituent substances.
The dose of the drug set individually, depending on the type of invasion and body weight of the patient.
The maximum daily dose is 800 mg.
Children should, if possible, avoid using high doses of albendazole for a long time.
With nematodoses (as well as ascariasis, trichocephalosis, necatoriasis)
The standard dose for treating roundworm invasions for adults and children weighing 60 kg or more is 400 mg per day, once;
for adults and children weighing less than 60 kg -15 mg / kg body weight once or in 2 doses.
In enterobiasis, adults and children over 3 years of age take the drug at a dose of 400 mg once. If necessary, after 14 days, repeat the course of treatment in the same dose and in the same regimen.
With strongyloidiasis, ankylostomiasis, adults and children over 3 years of age take the drug at a dose of 400 mg once a day for 3 days. If necessary, after 7 days, repeat the course of treatment in the same doses.
With trichinosis, the drug is taken on 400 mg 2 times a day for 10-14 days. In severe invasions and organ lesions (myocarditis, pneumonitis, meningoencephalitis), glucocorticosteroid and symptomatic agents are also taken.
With toxocarosis, adults and children over 14 years old and with a body weight of more than 60 kg take the drug at 400 mg 2 times a day for 10 days, with a body weight less than 60 kg 200 mg. Repeated courses of treatment with an interval of 2 weeks / month are required. During treatment, control of peripheral blood (once every 5-7 days) and aminotransferases at the same time is necessary.
When giardiasis: 400 mg 1 time per day for 3 days. For children weighing less than 10 kg -200 mg once a day, once for 5 days.
In case of mixed invasions, the drug is taken in 400 mg 2 times a day, for 3 days. If necessary, the treatment can be repeated after 1 month.
With neurocysticercosis and hydatid echinoccosis in patients with a body weight of 60 kg or more, take 400 mg 2 times a day, with a body weight less than 60 kg - at the rate of 15 mg / kg body weight per day in 2 doses; maximum daily dose of 800 mg. The course of treatment for neurocysticercosis is 28-30 days (2 days before taking the drug and the first week of taking glucocorticosteroid drugs), for echinococcosis - 3 cycles of 28 days with a 14 day break between cycles.
Before using the drug requires a clinical blood test and biochemical blood tests. The treatment is carried out at normal laboratory parameters. In the course of treatment, a study of blood and aminotransferases is conducted every 5-7 days.
With a decrease in leukocytes below 3.0x109 and a 2-fold increase in the activity of aminotransferases, it is necessary to suspend treatment until normalization of indicators.
Drug therapy can be resumed after laboratory indicators return to the same level as before the start of therapy; however, laboratory studies should be performed regularly during therapy.
The appointment of hepatoprotectors in the course of treatment and in cases of toxic manifestations is ineffective, the drug should be discontinued.
Treatment with albendazole for alveolar echinococcosis is an additional remedy.
Doses and mode of administration of the drug are the same as with hydatid echinococcosis. The duration and course of treatment is determined by the patient's condition and the tolerance of the drug.
On the part of the digestive system: abnormal liver function with a change in liver function tests (mild or moderate increase in liver transaminases), hepatitis, acute liver failure, epigastric pain, anorexia, constipation, diarrhea, and dry mouth. nausea, vomiting.
On the part of the hemopoietic system: inhibition of bone marrow hematopoiesis (leukopenia, granulocytopenia, agranulocytosis, thrombocytopenia, pancytopenia, aplastic anemia, suppression of bone marrow activity, neutropenia).
Since the cardiovascular system: increased blood pressure.
From the side of the central nervous system: headache and dizziness, meningeal symptoms, increased intracranial pressure.
On the part of the urinary system: a change in renal function (acute renal failure).
On the part of the skin: itching, skin rash, erythema multimorphic, Stevens-Johnson syndrome.
Allergic reactions: angioedema, immediate type hypersensitivity reactions.
Other: hyperthermia, alopecia.
If any of the side effects indicated in the instruction are aggravated, or you have noticed any other side effects not indicated in the instruction, inform your doctor.
- Hypersensitivity to albendazole, other components of the drug and other benzimidazole derivatives;
- Pathology of the retina;
- children's age up to 3 years (for this dosage form);
- pregnancy and breastfeeding period
The drug albendazole is used with caution in liver dysfunction (it is necessary to monitor liver function regularly before and during treatment), inhibition of bone marrow hematopoiesis, and liver cirrhosis.
The simultaneous use of albendazole with irazikvantel, dexamethasone and cimetidine can increase the concentration of albendazole sulfoxide in the blood. Simultaneous use with carbamazepine, phenytoin, phenobarbital and ginseng ordinary can lead to a decrease in the concentration of the drug albendazole in the intestine.
Pregnancy and Lactation
The drug albendazole is contraindicated during pregnancy and during breastfeeding.
It is recommended that simultaneous treatment of all family members.
Monitoring of blood cell composition is recommended; in the event of leukopenia, drug therapy is suspended.
In case of neurocysticercosis with eye lesions, before starting treatment, retinal examination is necessary due to the risk of aggravating its pathology.
In women of childbearing age, a pregnancy test is performed before starting treatment. During therapy and for 1 month after its completion, reliable contraception is necessary.
It should be remembered that before using Nemozole, like any other anthelmintic drug, you should carefully clean the room, wash children's toys, daily (morning and evening) hygiene, change of underwear. During treatment and several days after taking the drug, it is advisable to change bed linen more often or iron it with a hot iron.
The simultaneous use of albendazole and theophylline may lead to an increased risk of toxic effects of theophylline (nausea, vomiting, rapid heartbeat, seizures). Although single doses of albendazole do not inhibit theophylline metabolism, albendazole still induces cytochrome P4501A in hepatocytes. In this regard, it is recommended to monitor the plasma concentrations of theophylline during treatment with albendazole.
Patients should avoid eating grapefruit products while taking albendazole, since plasma concentrations of albendazole may increase, which increases the risk of adverse reactions.
Influence on ability to steer vehicles, mechanisms
You must avoid driving and engaging in other potentially dangerous activities that require increased concentration and psychomotor speed, as the drug can cause dizziness and other side effects that can affect these abilities.
Symptoms: increased dose-related side effects.
Treatment: gastric lavage, the use of Activated charcoal, symptomatic therapy.
- Brand name: Albendazole
- Active ingredient: Albendazole
- Dosage form: Pills.
- Manufacturer: Egis
- Country of Origin: Hungary
- Sulfamethazine, Sulfothiazole and Albendazole Residue Dosage in Food Products Determined by Liquid Chromatography/Tandem Mass Spectrometry
- Enantioselective analysis of albendazole sulfoxide in plasma using the chiral stationary phase
- Enantioselective kinetic disposition of albendazole sulfoxide in patients with neurocysticercosis
- Therapeutic drug monitoring of albendazole: Determination of albendazole, albendazole sulfoxide, and albendazole sulfone in human plasma using nonaqueous capillary electrophoresis
- Aplastic anemia during treatment with albendazole
- Enantioselective analysis of albendazole sulfoxide in cerebrospinal fluid by capillary electrophoresis
- Chiral analysis of albendazole sulfoxide enantiomers in human plasma and saliva using capillary electrophoresis with on-column absorption and fluorescence detection
- Methimazole increases the plasma concentrations of the albendazole metabolites of netobimin in sheep
- Dose dependent pharmacokinetics of albendazole in human
- Effect of amphiphilic surfactant agents on the gastrointestinal absorption of albendazole in cattle
- Time dependent pharmacokinetics of albendazole in human
- Pre-operative albendazole therapy for hydatid cyst
- Pre-operative albendazole therapy and hydatid cysts
- Combination chemotherapy is more effective in postspillage prophylaxis for hydatid disease than either albendazole or praziquantel alone
- Application of ultra-performance columns in high-performance liquid chromatography for determination of albendazole and its metabolites in turkeys
- Highly sensitive LC-MS/MS-ESI method for simultaneous quantitation of albendazole and ricobendazole in rat plasma and its application to a rat pharmacokinetic study
- A simple LC-MS/MS method to determine plasma and cerebrospinal fluid levels of albendazole metabolites (albendazole sulfoxide and albendazole sulfone) in patients with neurocysticercosis
- Enantioselective renal excretion of albendazole metabolites in patients with neurocysticercosis
- Direct separation of albendazole sulfoxide enantiomers by liquid chromatography on a chiral column deriving from (S)-N-(3,5-dinitrobenzoyl)tyrosine: application to enantiomeric assays on plasma samples
- Species differences in the generation of the chiral sulfoxide metabolite of albendazole in sheep and rats
- Spectrophotometric Determination of Albendazole Drug in Tablets: Spectroscopic Characterization of the Charge-transfer Solid Complexes
- Development of colon-targeted albendazole-β-cyclodextrin-complex drug delivery systems
- Pharmacokinetic evaluation and studies on the clinical efficacy of guar gum-–based oral drug delivery systems of albendazole and albendazole-β-cyclodextrin for colon-targeting in human volunteers
- Capillary electrophoresis and hollow fiber liquid-phase microextraction for the enantioselective determination of albendazole sulfoxide after biotransformation of albendazole by an endophytic fungus